Efaroxan (RX 821037) is a potent and selective alpha(2)-adrenoceptor antagonist. Additionally, Efaroxan is a selective antagonist at the imidazoline I1 receptor. Efaroxan promotes insulin secretion, in the absence of exogenous agonists, by a mechanism that involves inhibition of ATP-regulated K+ channels. Efaroxan was in clinical trials for the treatment of diabetes mellitus however its development has been discontinued.

FENFLUTHRIN, a synthetic pyrethroid, is an obsolete insecticide that was used to control a variety of insect pests in food stores and for public hygiene purposes.

Ursulcholic acid is a soluble form of ursodeoxycholic acid. It is an anticholinergic agent.

Revatropate is a muscarinic antagonist with selectivity for M1 and M3 receptor subtypes. Significant improvement in airway function was shown in horses with heaves after inhalation of revatropate, and it was found to be a safe and effective bronchodilator. Early clinical studies in chronic obstructive airway disease (COAD) patients also showed that inhaled revatropate was an effective bronchodilator, and well tolerated.

Fostedil (KB-944) is a phosphonic acid derivative with potent vasodilator activity. KB-944 has been demonstrated to produce long lasting coronary vasodilator and hypotensive effects in conscious and anesthetized dogs; increase coronary blood flow in isolated, blood perfused heart preparations of dogs; and reduce systemic pressure in conscious normotensive and hypertensive rats. Slow channel calcium entry blockade is thought to contribute to the vasodilator activity of KB-944. Fostedil is longer acting in hypertensive animals than either nifedipine or diltiazem suggesting a potential clinical advantage for this compound. Unexpectedly, fostedil was shown to produce atrial fibrillation in 3 of 10 hypertensive patients in a placebo controlled study. Fostedil had been in phase II clinical trials for the treatment of angina pectoris. However, this research has been discontinued.

LEMINOPRAZOLE is an inhibitor of the gastric mucosal proton pump. Its development for the treatment of peptic ulcer was discontinued.

Cetamolol is a beta adrenergic antagonist with intrinsic sympathomimetic activity, patented by Imperial Chemical Industries Ltd for cardiovascular disease treatment. The average plasma half-life of cetamolol is 6.4 hours in humans and peak serum levels are reached 1 to 2 hours after drug intake; oral doses as low as 10 mg produced significant reductions in exercise-induced tachycardia 24 hours after drug administration. Cetamolol is approximately three times as potent as atenolol in blocking exercise-induced tachycardia.

Linifanib (ABT-869) is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families, but has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) does not have a general antiproliferative effect due to its high dose requirement. However, it may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3). Linifanib (ABT-869) was in phase III clinical trial for the treatment of hepatocellular carcinoma, but the study failed to meet the primary end point.